KR101687084B1 - Hcv rna 복제의 억제제로서 4'-아지도, 3'-플루오로 치환된 뉴클레오시드 유도체 - Google Patents
Hcv rna 복제의 억제제로서 4'-아지도, 3'-플루오로 치환된 뉴클레오시드 유도체 Download PDFInfo
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- KR101687084B1 KR101687084B1 KR1020147020094A KR20147020094A KR101687084B1 KR 101687084 B1 KR101687084 B1 KR 101687084B1 KR 1020147020094 A KR1020147020094 A KR 1020147020094A KR 20147020094 A KR20147020094 A KR 20147020094A KR 101687084 B1 KR101687084 B1 KR 101687084B1
- Authority
- KR
- South Korea
- Prior art keywords
- rti
- tetrahydro
- furan
- hydroxy
- phosphorylamino
- Prior art date
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- 0 CC*CC(C)C(CCC(C)C1)C1C(C(C)CC=CC)C1C(CC(C)C(C)C2(*CC)C(*C)C2)CCC1 Chemical compound CC*CC(C)C(CCC(C)C1)C1C(C(C)CC=CC)C1C(CC(C)C(C)C2(*CC)C(*C)C2)CCC1 0.000 description 6
- HWPZZUQOWRWFDB-UHFFFAOYSA-N CN(C=CC(N)=N1)C1=O Chemical compound CN(C=CC(N)=N1)C1=O HWPZZUQOWRWFDB-UHFFFAOYSA-N 0.000 description 2
- PAIJFGAVPJOVTI-UHFFFAOYSA-N NC(C=CN1I)=NC1=O Chemical compound NC(C=CN1I)=NC1=O PAIJFGAVPJOVTI-UHFFFAOYSA-N 0.000 description 1
- IUWNKOFHRMMOIE-NETXQHHPSA-N N[C@@](CI)(CC1)OC1N(C=CC(N1)=O)C1=O Chemical compound N[C@@](CI)(CC1)OC1N(C=CC(N1)=O)C1=O IUWNKOFHRMMOIE-NETXQHHPSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
- C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
- C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
- C07H19/06—Pyrimidine radicals
- C07H19/10—Pyrimidine radicals with the saccharide radical esterified by phosphoric or polyphosphoric acids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
- A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
- A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
- A61K31/7068—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
- A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
- A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
- A61K31/7068—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
- A61K31/7072—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
- C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
- C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
- C07H19/06—Pyrimidine radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
- C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
- C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
- C07H19/16—Purine radicals
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Molecular Biology (AREA)
- Engineering & Computer Science (AREA)
- Genetics & Genomics (AREA)
- Biochemistry (AREA)
- Biotechnology (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Virology (AREA)
- General Chemical & Material Sciences (AREA)
- Oncology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Gastroenterology & Hepatology (AREA)
- Communicable Diseases (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Saccharide Compounds (AREA)
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201161577712P | 2011-12-20 | 2011-12-20 | |
US61/577,712 | 2011-12-20 | ||
PCT/EP2012/075688 WO2013092447A1 (en) | 2011-12-20 | 2012-12-17 | 4'-azido, 3'-fluoro substituted nucleoside derivatives as inhibitors of hcv rna replication |
Publications (2)
Publication Number | Publication Date |
---|---|
KR20140108303A KR20140108303A (ko) | 2014-09-05 |
KR101687084B1 true KR101687084B1 (ko) | 2016-12-15 |
Family
ID=47469968
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
KR1020147020094A KR101687084B1 (ko) | 2011-12-20 | 2012-12-17 | Hcv rna 복제의 억제제로서 4'-아지도, 3'-플루오로 치환된 뉴클레오시드 유도체 |
Country Status (31)
Country | Link |
---|---|
US (1) | US9708357B2 (el) |
EP (1) | EP2794628B1 (el) |
JP (1) | JP6118336B2 (el) |
KR (1) | KR101687084B1 (el) |
CN (2) | CN104011060A (el) |
AU (1) | AU2012357986B2 (el) |
BR (1) | BR112014015066A2 (el) |
CA (1) | CA2869317C (el) |
CL (1) | CL2014001599A1 (el) |
CO (1) | CO6990719A2 (el) |
CR (1) | CR20140255A (el) |
CY (1) | CY1119015T1 (el) |
DK (1) | DK2794628T3 (el) |
EA (1) | EA024847B1 (el) |
ES (1) | ES2626484T3 (el) |
HK (2) | HK1199037A1 (el) |
HU (1) | HUE033332T2 (el) |
IL (1) | IL232843B (el) |
IN (1) | IN2014CN04530A (el) |
LT (1) | LT2794628T (el) |
MA (1) | MA35749B1 (el) |
MX (1) | MX350810B (el) |
PE (1) | PE20141599A1 (el) |
PH (1) | PH12014501283A1 (el) |
PL (1) | PL2794628T3 (el) |
PT (1) | PT2794628T (el) |
SG (1) | SG11201403086YA (el) |
SI (1) | SI2794628T1 (el) |
UA (1) | UA110428C2 (el) |
WO (1) | WO2013092447A1 (el) |
ZA (1) | ZA201404444B (el) |
Families Citing this family (20)
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EP2755983B1 (en) | 2011-09-12 | 2017-03-15 | Idenix Pharmaceuticals LLC. | Substituted carbonyloxymethylphosphoramidate compounds and pharmaceutical compositions for the treatment of viral infections |
DK2794628T3 (en) | 2011-12-20 | 2017-07-10 | Riboscience Llc | 4'-AZIDO-3'-FLUORO-SUBSTITUTED NUCLEOSIDE DERIVATIVES AS INHIBITORS OF HCV RNA REPLICATION |
EP2852605B1 (en) | 2012-05-22 | 2018-01-31 | Idenix Pharmaceuticals LLC | 3',5'-cyclic phosphate prodrugs for hcv infection |
US9109001B2 (en) | 2012-05-22 | 2015-08-18 | Idenix Pharmaceuticals, Inc. | 3′,5′-cyclic phosphoramidate prodrugs for HCV infection |
AU2013266393B2 (en) | 2012-05-22 | 2017-09-28 | Idenix Pharmaceuticals Llc | D-amino acid compounds for liver disease |
AR091156A1 (es) | 2012-05-25 | 2015-01-14 | Jansen R & D Ireland | Nucleosidos de espirooxetano de uracilo |
EP2900682A1 (en) | 2012-09-27 | 2015-08-05 | IDENIX Pharmaceuticals, Inc. | Esters and malonates of sate prodrugs |
MX353422B (es) | 2012-10-08 | 2018-01-12 | Idenix Pharmaceuticals Llc | Análogos de 2'-cloronucleósido para infección por vhc. |
EP2909222B1 (en) | 2012-10-22 | 2021-05-26 | Idenix Pharmaceuticals LLC | 2',4'-bridged nucleosides for hcv infection |
US9211300B2 (en) | 2012-12-19 | 2015-12-15 | Idenix Pharmaceuticals Llc | 4′-fluoro nucleosides for the treatment of HCV |
WO2014137926A1 (en) | 2013-03-04 | 2014-09-12 | Idenix Pharmaceuticals, Inc. | 3'-deoxy nucleosides for the treatment of hcv |
US9339541B2 (en) | 2013-03-04 | 2016-05-17 | Merck Sharp & Dohme Corp. | Thiophosphate nucleosides for the treatment of HCV |
EP2970357A1 (en) | 2013-03-13 | 2016-01-20 | IDENIX Pharmaceuticals, Inc. | Amino acid phosphoramidate pronucleotides of 2'-cyano, azido and amino nucleosides for the treatment of hcv |
EP2981542B1 (en) | 2013-04-01 | 2021-09-15 | Idenix Pharmaceuticals LLC | 2',4'-fluoro nucleosides for the treatment of hcv |
EA201592185A1 (ru) * | 2013-05-16 | 2016-05-31 | Рибосайенс Ллк | 4'-азидо, 3'-дезокси-3'-фторзамещенные нуклеозидные производные |
EP3004130B1 (en) | 2013-06-05 | 2019-08-07 | Idenix Pharmaceuticals LLC. | 1',4'-thio nucleosides for the treatment of hcv |
WO2015017713A1 (en) | 2013-08-01 | 2015-02-05 | Idenix Pharmaceuticals, Inc. | D-amino acid phosphoramidate pronucleotides of halogeno pyrimidine compounds for liver disease |
WO2015161137A1 (en) | 2014-04-16 | 2015-10-22 | Idenix Pharmaceuticals, Inc. | 3'-substituted methyl or alkynyl nucleosides for the treatment of hcv |
CN108350016B (zh) * | 2015-09-02 | 2021-07-27 | 艾伯维公司 | 抗病毒四氢呋喃衍生物 |
WO2020007070A1 (zh) * | 2018-07-02 | 2020-01-09 | 河南真实生物科技有限公司 | 4'-取代核苷的晶型、制备和应用 |
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2012
- 2012-12-17 DK DK12808791.3T patent/DK2794628T3/en active
- 2012-12-17 SI SI201230977A patent/SI2794628T1/sl unknown
- 2012-12-17 ES ES12808791.3T patent/ES2626484T3/es active Active
- 2012-12-17 EP EP12808791.3A patent/EP2794628B1/en not_active Not-in-force
- 2012-12-17 CA CA2869317A patent/CA2869317C/en not_active Expired - Fee Related
- 2012-12-17 JP JP2014547882A patent/JP6118336B2/ja active Active
- 2012-12-17 SG SG11201403086YA patent/SG11201403086YA/en unknown
- 2012-12-17 LT LTEP12808791.3T patent/LT2794628T/lt unknown
- 2012-12-17 WO PCT/EP2012/075688 patent/WO2013092447A1/en active Application Filing
- 2012-12-17 CN CN201280064193.6A patent/CN104011060A/zh active Pending
- 2012-12-17 PL PL12808791T patent/PL2794628T3/pl unknown
- 2012-12-17 US US14/366,189 patent/US9708357B2/en not_active Expired - Fee Related
- 2012-12-17 IN IN4530CHN2014 patent/IN2014CN04530A/en unknown
- 2012-12-17 AU AU2012357986A patent/AU2012357986B2/en not_active Ceased
- 2012-12-17 CN CN201810341927.XA patent/CN108409820A/zh not_active Withdrawn
- 2012-12-17 UA UAA201408090A patent/UA110428C2/uk unknown
- 2012-12-17 HU HUE12808791A patent/HUE033332T2/en unknown
- 2012-12-17 BR BR112014015066A patent/BR112014015066A2/pt not_active IP Right Cessation
- 2012-12-17 PT PT128087913T patent/PT2794628T/pt unknown
- 2012-12-17 PE PE2014000990A patent/PE20141599A1/es not_active Application Discontinuation
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WO2002100415A2 (en) | 2001-06-12 | 2002-12-19 | F. Hoffmann-La Roche Ag | 4'-substituted nucleosides for the treatment of diseases mediated by the hepatitis c virus |
WO2012040124A1 (en) | 2010-09-22 | 2012-03-29 | Alios Biopharma, Inc. | Azido nucleosides and nucleotide analogs |
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